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11. 发明申请

WO2011076811A1 CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS 审中-公开
标题翻译：羧酰胺化合物及其作为钙蛋白酶抑制剂的用途
公开(公告)号：WO2011076811A1
公开(公告)日：2011-06-30
申请号：PCT/EP2010/070418
申请日：2010-12-21
申请人： ABBOTT GMBH & CO. KG , ABBOTT LABORATORIES , KLING, Andreas , JANTOS, Katja , MACK, Helmut , MÖLLER, Achim , HORNBERGER, Wilfried , BACKFISCH, Gisela , LAO, Yanbin , NIJSEN, Marjoleen
发明人： KLING, Andreas , JANTOS, Katja , MACK, Helmut , MÖLLER, Achim , HORNBERGER, Wilfried , BACKFISCH, Gisela , LAO, Yanbin , NIJSEN, Marjoleen
IPC分类号： C07D207/28 , C07D401/04 , C07D401/14 , C07D417/14 , A61K31/4015 , A61K31/4439 , A61P25/28 , A61P27/08 , A61P35/00 , A61P13/12 , A61P31/00 , A61P31/18 , A61P25/00 , A61P9/00 , A61P21/00
CPC分类号： C07D401/04 , C07D207/28 , C07D401/14 , C07D409/14 , C07D417/14
摘要： The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R 1 , R 2 , R 3 R 4 , R 5 , m and n have the meanings mentioned in the claims and the description, the tautomers thereof, the hydrates thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein R 1 is optionally substituted phenyl-C 1 -C 2 -alkyl or hetaryl-C 1 -C 2 -alkyl, R 2 is optionally substituted aryl, hetaryl, aryl-C 1 -C 6 -alkyl, aryl-C 2 -C 6 -alkenyl or hetaryl-C 1 -C 4 -alkyl, R 3 is C 1 -C 3 -alkyl, C 1 -C 3 -haloalkyl, C 2 -C 4 -alkenyl, C 3 -C 6 -cycloalkyl, C 3 -C 6 -cycloalkyl-C 1 -C 2 -alkyl, or phenyl-C 1 -C 3 -alkyl, R 4 and R 5 independently of one another are halogen, CF 3 , CHF 2 , CH 2 F, C 1 -C 2 -alkyl or C 1 -C 2 -alkoxy, and m and n independently of one another are 0 or 1.
摘要翻译：本发明涉及新的羧酰胺化合物及其用于制备药物的用途。羧酰胺化合物是钙蛋白酶（钙依赖性半胱氨酸蛋白酶）的抑制剂。因此，本发明还涉及这些羧酰胺化合物用于治疗与升高的钙蛋白酶活性相关的病症的用途。羧酰胺化合物是通式I的化合物，其中R 1，R 2，R 3，R 4，R 5，m和n具有权利要求书和描述中所述的含义，其互变异构体，其水合物及其药学上合适的盐。在这些化合物中，优选其中R 1为任选取代的苯基-C 1 -C 2 - 烷基或杂芳基-C 1 -C 2烷基，R 2为任选取代的芳基，杂芳基，芳基-C 1 -C 6 - 烷基，芳基-C 2 -C 6 - 烯基或杂芳基-C 1 -C 4 - 烷基，R 3是C 1 -C 3 - 烷基，C 1 -C 3 - 卤代烷基，C 2 -C 4 - 烯基，C 3 -C 6 - 环烷基，C 3 -C 6 - 环烷基-C 1 -C 2烷基或苯基 - C 1 -C 3 - 烷基，R 4和R 5彼此独立地是卤素，CF 3，CHF 2，CH 2 F，C 1 -C 2 - 烷基或C 1 -C 2 - 烷氧基，m和n彼此独立地为0或1。

12. 发明申请

WO2010094755A1 CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS 审中-公开
标题翻译：羧酰胺化合物及其作为钙蛋白酶抑制剂的用途
公开(公告)号：WO2010094755A1
公开(公告)日：2010-08-26
申请号：PCT/EP2010/052102
申请日：2010-02-19
申请人： ABBOTT GMBH & CO. KG , KLING, Andreas , MACK, Helmut , JANTOS, Katja , MOELLER, Achim , HORNBERGER, Wilfried , HUTCHINS, Charles, W. , ABBOTT LABORATORIES
发明人： KLING, Andreas , MACK, Helmut , JANTOS, Katja , MOELLER, Achim , HORNBERGER, Wilfried , HUTCHINS, Charles, W.
IPC分类号： C07D277/22 , C07D401/04 , C07D413/04 , C07D417/04 , A61K31/4439 , A61P25/00 , A61P35/00 , A61P31/18
CPC分类号： C07D417/04 , C07D277/30 , C07D401/04 , C07D413/04
摘要： The present invention relates to novel carboxamide compounds and their use as a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity and to a method for the therapeutic and/or prophylactic treatment by administering an effective amount of at least one of these carboxamide compounds. The carboxamide compounds are compounds of the general formula (I) in which W-R 2 is selected from formulae (1), (2) and (3) and R 1 , R 2 , R 3a , R 3b , Y 1 , Y 2 , Y 3 , Y 4 , X, Q, m, k, R w and R w* have the meanings mentioned in the claims, the tautomers thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein Y 1 , Y 2 , Y 3 and Y 4 are CR y , or one or two of the variables Y 1 to Y 4 are a nitrogen atom and the remaining variables are CR y , wherein the radicals Ry may be identical or different and have the meanings mentionend in the claims.
摘要翻译：本发明涉及新的羧酰胺化合物及其作为药物的用途。羧酰胺化合物是钙蛋白酶（钙依赖性半胱氨酸蛋白酶）的抑制剂。因此，本发明还涉及这些羧酰胺化合物用于治疗与钙蛋白酶活性升高相关的疾病的用途，以及通过施用有效量的这些羧酰胺化合物中的至少一种来进行治疗和/或预防性治疗的方法。羧酰胺化合物是通式（I）的化合物，其中W-R2选自式（1），（2）和（3），R1，R2，R3a，R3b，Y1，Y2，Y3，Y4，X ，Q，m，k，Rw和Rw *具有权利要求书中提及的含义，其互变异构体及其药学上合适的盐。在这些化合物中，优选其中Y1，Y2，Y3和Y4为CRy，或变量Y1至Y4中的一个或两个为氮原子，剩余的变量为CRy，其中基团Ry可以相同或不同，并且具有意思是在权利要求中提及。

13. 发明申请

WO2008009942A1 HETEROAROMATIC-BASED PEPTIDE MACROCYCLES AS G-QUADRUPLEX LIGANDS 审中-公开
标题翻译：作为G-QUADRUPLEX LIGANDS的基于异种基团的肽
公开(公告)号：WO2008009942A1
公开(公告)日：2008-01-24
申请号：PCT/GB2007/002734
申请日：2007-07-19
申请人： CAMBRIDGE ENTERPRISE LTD. , BALASUBRAMANIAN, Shankar , JANTOS, Katja , LADAME, Sylvain
发明人： BALASUBRAMANIAN, Shankar , JANTOS, Katja , LADAME, Sylvain
IPC分类号： C07K5/12 , A61P35/00
CPC分类号： A61K38/12 , C07D498/22 , Y02A50/395
摘要： This invention pertains generally to the field of G-quadruplex ligands, and more particularly, to certain heteroaromatic-based peptide macrocycles (HBPMs) of the following formula which, inter alia , (selectively) bind (and stabilize) G-quadruplexes formula (I): wherein: n is independently 0 or 1; each of Het 1 , Het 2 , Het 3 , and Het 4 if present, is independently a heteroaromatic 5-membered ring having exactly one ring heteroatom or exactly two ring heteroatoms, wherein each of said ring heteroatoms is independently selected from: nitrogen, oxygen, and sulphur (e.g., oxazole-di-yl and thiazole-di-yl); and is independently unsubstituted or substituted; each of R C1 , R C2 , R C3 , and R C4 is independently -H or a ring-carbon subsituent; and each of R N1 , R N2 , R N3 , and R N4 is independently -H or a ring-nitrogen subsituent. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo , to (selectively) bind (and stabilize) G-quadruplexes, to inhibit telomerase, to regulate cell proliferation, and in the treatment of proliferative conditions, such as cancer.
摘要翻译：本发明一般涉及G-四链体配体领域，更具体地说涉及下列通式的某些基于杂芳基的肽大环化合物（HBPM），其特别是（选择性地）结合（并稳定）G-四链体配方（I ）：其中：n独立地为0或1; Het 2，Het 3，Het 3，Het 4和Het 4如果存在，独立地是杂芳族5 其中每个所述环杂原子独立地选自：氮，氧和硫（例如恶唑二基和噻唑二基）;其中每个环杂原子具有一个环杂原子或正好两个环杂原子。并且独立地是未取代的或取代的; R C1，R C2和R C4各自独立地为-H或环 - 碳取代; 并且R“N”，“N”，“N”和“R”中的每一个独立地是-H或环 - 氮取代。本发明还涉及包含这种化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途（选择性地）结合（并稳定）G-四链体，抑制端粒酶调节细胞增殖，和治疗增生性疾病如癌症。

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